SC79

A cell-permeable and blood-brain barrier permeant bromo-to-chloro substituted HA14-1 analog that renders Akt in a conformation susceptible to phosphorylation by upstream kinases via specific interaction with Akt pleckstrin homology (PH) domain PtdIns(3,4,5)P3- (PIP3) binding pocket. Shown to enhance both basal and receptor-mediated Akt phosphorylation (Thr308 and Ser473) in a time- and dose-dependent manner (2 to 4 µg/ml) with concomitant inhibition Akt membrane translocation in various cell cultures. Efficiently reduces glutamate-induced neurotoxicity both in primary neuron cultures (EC₅₀ = 4 µg/ml) in vitro and in a murine MCAO (middle cerebral artery occlusion) model (40 mg/kg, i.p.) in vivo.

Cell permeable: yes

Primary Target
Pleckstrin homology (PH) domain of Akt

Packaged under inert gas

Following reconstitution, aliquot and immediately freeze (-70°C). Stock solutions are stable for up to 2 weeks at -70°C.

Use only fresh DMSO for reconstitution.

Jo. H., et al. 2012. Proc. Natl. Acad. Sci. USA109, 10581.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)